[关键词]
[摘要]
目的 研究薰鲁香Pistacia lentiscus的化学成分及其体外抗炎活性。方法 综合运用开放硅胶、MCI、ODS、Sephadex LH-20凝胶及半制备型高效液相色谱等技术进行分离,依据HR-ESI-MS、IR、NMR、ECD等谱学技术鉴定化合物结构。采用CCK-8法筛选化合物对小鼠单核巨噬细胞RAW264.7的细胞毒性,通过脂多糖(lipopolysaccharide,LPS)诱导的RAW264.7细胞炎症模型对更低无毒性剂量化合物进行抗炎活性评价。结果 从薰鲁香中分离得到7个化合物,分别鉴定为13β-hydroxy-3-oxo-1,11-dien-28-oic acid(1)、11α,12α-epoxy-3,4-seco-olean-4(23)-en-13β,28-dihydroxy-3-oic acid(2)、22-oxo-20-taraxasten-3β-ol(3)、3,11-dioxoolean-12-en-28-oic acid(4)、krukovines A(5)、erythrodiol(6)、11-oxoerythrodiol(7),其中化合物1和2为新化合物。化合物4(40 μmol/L)对RAW264.7细胞显示出明显的细胞毒性,化合物1~3、5、6对LPS诱导下RAW264.7细胞释放NO具有一定的抑制作用,IC50值在(16.89±0.98)~(27.33±1.25)μmol/L,弱于阳性对照地塞米松[(11.27±2.25)μmol/L]。结论 化合物1、2为新齐墩果烷型三萜,分别命名为薰鲁香三萜酸A(1)和开环薰鲁香三萜酸B(2);化合物3、6、7为首次从该植物分离得到;化合物1~3、5、6表现出一定的抗炎活性。
[Key word]
[Abstract]
Objective To investigate the chemical constituents of Pistacia lentiscus and their anti-inflammatory activities in vitro. Methods The compounds were isolated and purified by using a various silica gel, ODS, Sephadex LH-20, and prep HPLC, and their structures were elucidated by HR-ESI-MS, IR, NMR. Screening of cytotoxicity of all compounds to RAW264.7 cells using the CCK-8 method, and evaluate the anti-inflammatory activity of low toxicity compounds through the RAW264.7 cell inflammatory model induced by lipopolysaccharide (LPS). Results Seven compounds were isolated from mastic and identified as13β-hydroxy-3-oxo-1,11-dien-28-oic acid (1), 11α,12α-epoxy-3,4-seco-olean-4(23)-en-13β,28-dihydroxy-3-oic acid (2), 22-oxo-20-taraxasten-3β-ol (3), 3,11-dioxoolean-12-en-28-oicacid (4), krukovines A (5), erythrodiol (6), 11-oxoerythrodiol (7). Compound 4 (40 μmol/L) showed significant cytotoxicity to RAW264.7 cells, while compounds 1—3, 5 and 6 exhibited a certain inhibitory effect on the release of NO by RAW264.7 cells induced by LPS with IC50 value ranging from (16.89 ± 0.98) to (27.33 ± 1.25) μmol/L, which were weaker than the positive control dexamethasone (11.27 ± 2.25) μmol/L. Conclusion Compounds 1 and 2 are new oleanane-type triterpenes named mastriterpenoid acid A and secomastriterpenoid acid B, and compounds 3, 6 and 7 were first isolated from the plant. Compounds 1—3, 5 and 6 exhibit certain anti-inflammatory activity.
[中图分类号]
R284.1
[基金项目]
国家自然科学基金资助项目(82060774);天然与仿生药物研究江西省重点实验室开放课题(2024SSY07051)